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Synthetic studies and pharmacological evaluations on the MDMA (‘Ecstasy’) antagonist nantenine

Synthetic studies and pharmacological evaluations on the MDMA (‘Ecstasy’) antagonist nantenine

  1. Anonymous
    Bioorganic & Medicinal Chemistry Letters 20 (2010) 628–631
    LeGendre et al.

    The naturally occurring aporphine alkaloid nantenine, has been shown to antagonize behavioral and
    physiological effects of MDMA in mice. We have synthesized (±)-nantenine via an oxidative cyclization
    reaction with PIFA and evaluated its binding profile against a panel of CNS targets. To begin to understand the importance of the chiral center of nantenine with regards to its capacity to antagonize the effects of MDMA in vivo, (R)- and (S)-nantenine were prepared and evaluated in a food-reinforced operant task in rats. Pretreatment with either nantenine enantiomer (0.3 mg/kg ip) completely blocked the behavioral suppression induced upon administration of 3.0 mg/kg MDMA. (±)-Nantenine displayed high affinity and selectivity for the a1A adrenergic receptor among several other receptors suggesting that this a1 subtype may be significantly involved in the anti-MDMA effects of the enantiomers.